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    • 7. 发明授权
    • Piperazine compounds as inhibitors of MMP or TNF
    • 哌嗪化合物作为MMP或TNF的抑制剂
    • US06333324B1
    • 2001-12-25
    • US09319928
    • 1999-07-26
    • Masahiro NeyaHitoshi YamazakiNatsuko KayakiriKentaro SatoTeruo Oku
    • Masahiro NeyaHitoshi YamazakiNatsuko KayakiriKentaro SatoTeruo Oku
    • C07D24104
    • C07D405/12C07D241/04C07D405/14C07D409/12C07D409/14C07D413/14C07D417/12C07D417/14
    • A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a medicament for prophylactic and therapeutic treatment of MMP- or TNF&agr;-mediated diseases.
    • 式(I)的化合物,其中A是磺酰基或羰基; R1是任选取代的芳基,任选取代的杂环基,任选取代的低级烷基或任选取代的低级烯基; R2是氢,任选取代的低级烷基,任选取代的芳基或任选取代的杂环基; R 3是任选取代的低级烷基,任选取代的低级烷氧基,任选取代的芳氧基,任选取代的低级烯基,任选取代的芳基,任选取代的杂环基或任选取代的氨基; R4是氢,任选取代的低级烷基,任选取代的芳基或任选取代的杂环基; R5是氢,任选取代的低级烷基,任选取代的芳基或任选取代的杂环基; R 10为羟基或被保护的羟基及其药学上可接受的盐。 本发明的化合物可用作用于预防和治疗MMP或TNFα介导的疾病的药物。